Dosing regimens for lasofoxifene

• US 6,436,977 B1
• Filed: 09/06/2000
• Issued: 08/20/2002
• Est. Priority Date: 09/29/1999
• Status: Expired due to Term

• Current Assignee: Pfizer Inc.
• Original Assignee: Pfizer Inc.
• Inventors: Thompson, David D.
• Primary Examiner(s): Fay, Zohreh
• Assistant Examiner(s): KWON, YONG SOK
• Application Number:
  US09/656,273
• Time in Patent Office: 713 Days
• Field of Search: 514/367, 514/377
• US Class Current: 514/367
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 19/10 for osteoporosis
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/04 specific for metastasis
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: A61P 5/32 Antioestrogens
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Based on lasofoxifene'"'"'s half-life and potency, the drug may be dosed once per week and achieve a similar effect as if given daily.

Claims

1. A method of administering (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol or a pharmacologically acceptable salt thereof to a patient in need thereof, the method comprising administering a single dose, which dose results in a blood concentration of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol or a pharmacologically acceptable salt thereof of greater than about 0.3 ng/ml over an extended period of time wherein, the extended period of time is from about seven days to about thirty days.

2. The method of claim 1 wherein the single dose is about 0.8 to about 10.0 mg.

3. The method of claim 1 wherein the single dose is about 10.0 to about 20.0 mg.

4. The method of claim 1 wherein the single dose is about 0.8 mg and the extended period of time is about seven days.

5. The method of claim 1 wherein the single dose is about 10.0 mg and the extended period of time is about 30 days.

6. The method of claim 1 wherein the single dose is administered orally.

7. The method of claim 1 wherein the single dose is about 0.8 to about 20.0 mg and the extended period of time is about seven to about 30 days.

8. The method of claim 1 wherein the (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol or a pharmacologically acceptable salt thereof is (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol, D-tartrate.